[go: up one dir, main page]

PE20150767A1 - Inhibidores de gdf-8 - Google Patents

Inhibidores de gdf-8

Info

Publication number
PE20150767A1
PE20150767A1 PE2015000455A PE2015000455A PE20150767A1 PE 20150767 A1 PE20150767 A1 PE 20150767A1 PE 2015000455 A PE2015000455 A PE 2015000455A PE 2015000455 A PE2015000455 A PE 2015000455A PE 20150767 A1 PE20150767 A1 PE 20150767A1
Authority
PE
Peru
Prior art keywords
indazole
pyridin
ethoxy
inhibitors
independently
Prior art date
Application number
PE2015000455A
Other languages
English (en)
Inventor
Somasekhar Bhamidipati
Marina Gelman
Pingyu Ding
Rajinder Singh
Jeffrey Clough
Todd Kinsella
Donald Payan
Original Assignee
Rigel Pharmaceuticals Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=49474701&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20150767(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Rigel Pharmaceuticals Inc filed Critical Rigel Pharmaceuticals Inc
Publication of PE20150767A1 publication Critical patent/PE20150767A1/es

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/02—Nutrients, e.g. vitamins, minerals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/18—Drugs for disorders of the endocrine system of the parathyroid hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/26—Androgens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/44—Glucocorticosteroids; Drugs increasing or potentiating the activity of glucocorticosteroids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/26—Radicals substituted by halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6503—Five-membered rings
    • C07F9/65031—Five-membered rings having the nitrogen atoms in the positions 1 and 2
    • C07F9/65038—Five-membered rings having the nitrogen atoms in the positions 1 and 2 condensed with carbocyclic rings or carbocyclic ring systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Rheumatology (AREA)
  • Nutrition Science (AREA)
  • Neurology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Emergency Medicine (AREA)
  • Pulmonology (AREA)
  • Reproductive Health (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Epidemiology (AREA)

Abstract

La invencion describe inhibidores de GCF-8 de la formula (I), y sus sales farmaceuticamente aceptables, en donde n es 1-4; R1y R2 son cada uno, de modo independiente, H, halogeno, nitro, entre otros; R5 y R6 son cada uno, de modo independiente, H, alquilo C1-C6, haloalquilo C1-C6, entre otros; X es N y Z es un anillo biciclico fusionado. Tambien se proporcionan composiciones farmaceuticas que los comprenden. Estos compuestos y composiciones son utiles en metodos para inhibir GDF-8 en una celula y metodos para tratar a un paciente que sufre de una enfermedad o trastorno, en donde el paciente se beneficiaria de un aumento de masa o fuerza de tejido muscular. Los compuestos preferidos son: 5-(5-Etoxi-2-(4-fluoro-3-metilfenil)piridin-3-il)-1H-indazol; 5-(5-Etoxi-2-(2-fluorofenil)piridin-3-il)-1H-indazol; entre otros
PE2015000455A 2012-10-05 2013-10-04 Inhibidores de gdf-8 PE20150767A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201261710449P 2012-10-05 2012-10-05

Publications (1)

Publication Number Publication Date
PE20150767A1 true PE20150767A1 (es) 2015-05-15

Family

ID=49474701

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2015000455A PE20150767A1 (es) 2012-10-05 2013-10-04 Inhibidores de gdf-8

Country Status (20)

Country Link
US (3) US9145433B2 (es)
EP (1) EP2903978B1 (es)
JP (2) JP6457942B2 (es)
KR (1) KR20150072412A (es)
CN (1) CN104837832B (es)
AU (1) AU2013326867B2 (es)
BR (1) BR112015007182A2 (es)
CA (1) CA2887203A1 (es)
CL (1) CL2015000851A1 (es)
EA (1) EA201590693A1 (es)
IL (1) IL238031A0 (es)
MA (1) MA38050B1 (es)
MX (1) MX2015004151A (es)
PE (1) PE20150767A1 (es)
PH (1) PH12015500719A1 (es)
SA (1) SA515360229B1 (es)
SG (1) SG11201502527UA (es)
TN (1) TN2015000121A1 (es)
WO (1) WO2014055955A1 (es)
ZA (1) ZA201503041B (es)

Families Citing this family (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6457942B2 (ja) * 2012-10-05 2019-01-23 ライジェル ファーマシューティカルズ， インコーポレイテッド Ｇｄｆ−８阻害剤
PH12020552066A1 (en) 2014-02-13 2022-05-11 Incyte Corp Cyclopropylamines as lsd1 inhibitors
RS59534B1 (sr) 2014-02-13 2019-12-31 Incyte Corp Ciklopropilamini kao lsd1 inhibitori
US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
ES2759240T3 (es) 2014-04-08 2020-05-08 Rigel Pharmaceuticals Inc Compuestos de piridina 2,3-disustituidos como inhibidores de TGF-beta
SG11201608658SA (en) 2014-04-22 2016-11-29 Univ Basel Novel manufacturing process for triazine, pyrimidine and pyridine derivatives
CN103965192B (zh) * 2014-05-20 2016-01-13 定陶县友帮化工有限公司 一种6-氯咪唑并[1,2-a]吡啶-3-甲酸的合成方法
CN103965190A (zh) * 2014-05-20 2014-08-06 定陶县友帮化工有限公司 一种咪唑并[1,2-a]吡啶-3-甲酸的合成方法
CN103965191A (zh) * 2014-05-20 2014-08-06 定陶县友帮化工有限公司 一种6-溴咪唑并[1,2-a]吡啶-3-甲酸的合成方法
CA2953177C (en) 2014-06-23 2019-07-23 Dr. Reddy's Laboratories Ltd. Substituted imidazo[1,2-a]pyridine compounds useful for the treatment of pain
TWI687419B (zh) 2014-07-10 2020-03-11 美商英塞特公司 作為ｌｓｄ１抑制劑之咪唑并吡啶及咪唑并吡嗪
WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
WO2016007736A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Imidazopyrazines as lsd1 inhibitors
CN104402881B (zh) * 2014-11-05 2016-04-20 定陶县友帮化工有限公司 一种3-醛基-6-溴咪唑并[1,2-a]吡啶-8-甲酸乙酯的合成方法
ES2928084T3 (es) 2015-02-20 2022-11-15 Rigel Pharmaceuticals Inc Inhibidores de GDF-8
ES2789331T3 (es) 2015-03-02 2020-10-26 Rigel Pharmaceuticals Inc Inhibidores de TGF-beta
EP3626720A1 (en) 2015-04-03 2020-03-25 Incyte Corporation Heterocyclic compounds as lsd1 inhibitors
RS62639B1 (sr) 2015-07-06 2021-12-31 Alkermes Inc Hetero-halo inhibitori histonskih deacetilaza
EP3319968A1 (en) 2015-07-06 2018-05-16 Rodin Therapeutics, Inc. Heterobicyclic n-aminophenyl-amides as inhibitors of histone deacetylase
MX389824B (es) 2015-08-12 2025-03-20 Incyte Holdings Corp Sales de un inhibidor de dimetilasa 1 especifica para lisina (lsd1).
HK1255330A1 (zh) 2015-08-26 2019-08-16 缆图药品公司 适用於治疗与ntrk相关的病症的化合物和组合物
BR112018010024A8 (pt) * 2015-11-19 2019-02-26 Blueprint Medicines Corp compostos e composições úteis no tratamento de distúrbios relacionados a ntrk
ES3011058T3 (en) * 2015-11-25 2025-04-07 Convergene Llc Bicyclic bet bromodomain inhibitors and uses thereof
US11352328B2 (en) 2016-07-12 2022-06-07 Arisan Therapeutics Inc. Heterocyclic compounds for the treatment of arenavirus
EP3928784A1 (en) 2016-07-15 2021-12-29 Acceleron Pharma Inc. Compositions comprising actriia polypeptides for use in treating pulmonary hypertension
WO2018017633A1 (en) 2016-07-21 2018-01-25 Bristol-Myers Squibb Company TGF Beta RECEPTOR ANTAGONISTS
US11466003B2 (en) * 2016-07-29 2022-10-11 Shanghai Yingli Pharmaceutical Co., Ltd Nitrogenous heterocyclic aromatic compound, preparation method therefor, pharmaceutical composition thereof, and application thereof
WO2018049191A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyridone derivatives as hpk1 modulators and uses thereof for the treatment of cancer
US20180072718A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyridine compounds and uses thereof
TWI867311B (zh) 2016-09-09 2024-12-21 美商英塞特公司 吡唑并吡啶化合物及其用途
WO2018049152A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyrimidine derivatives as hpk1 modulators and uses thereof for the treatment of cancer
US11491025B2 (en) 2016-10-25 2022-11-08 Elevation Spine, Inc. Intervertebral implant and method of use
US10961239B2 (en) 2017-01-05 2021-03-30 Bristol-Myers Squibb Company TGF beta receptor antagonists
TWI770104B (zh) 2017-01-11 2022-07-11 美商羅登醫療公司 組蛋白去乙醯酶雙環抑制劑
US20180228786A1 (en) 2017-02-15 2018-08-16 Incyte Corporation Pyrazolopyridine compounds and uses thereof
AU2018291501B2 (en) 2017-06-30 2024-05-02 Elevation Spine, Inc. Interbody spacer and bone plate assembly, instrumentation, and methods
PL3664802T3 (pl) 2017-08-07 2022-07-11 Alkermes, Inc. Bicykliczne inhibitory deacetylaz histonowych
WO2019051199A1 (en) 2017-09-08 2019-03-14 Incyte Corporation 6-CYANO-INDAZOLE COMPOUNDS AS HEMATOPOIETIC PROGENITOR KINASE 1 (HPK1) MODULATORS
US10752635B2 (en) 2018-02-20 2020-08-25 Incyte Corporation Indazole compounds and uses thereof
US10745388B2 (en) 2018-02-20 2020-08-18 Incyte Corporation Indazole compounds and uses thereof
PE20210397A1 (es) 2018-02-20 2021-03-02 Incyte Corp Derivados de n-(fenil)-2-(fenil)pirimidina-4-carboxamida y compuestos relacionados como inhibidores hpki para tratar el cancer
US11299473B2 (en) 2018-04-13 2022-04-12 Incyte Corporation Benzimidazole and indole compounds and uses thereof
US10899755B2 (en) 2018-08-08 2021-01-26 Incyte Corporation Benzothiazole compounds and uses thereof
US10968200B2 (en) 2018-08-31 2021-04-06 Incyte Corporation Salts of an LSD1 inhibitor and processes for preparing the same
ES2973117T3 (es) 2018-09-25 2024-06-18 Incyte Corp Compuestos de pirazolo[4,3-d]pirimidina como moduladores de ALK2 y/o FGFR
US12419865B2 (en) 2018-12-06 2025-09-23 Arisan Therapeutics Inc. Compounds for the treatment of arenavirus infection
MX2021013135A (es) 2019-04-29 2021-11-25 Solent Therapeutics Llc Derivados de 1,1-dioxido de 3-amino-4h-benzo[e][1,2,4] tiadiazina como inhibidores de mrgx2.
TWI865579B (zh) 2019-08-06 2024-12-11 美商英塞特公司 Ｈｐｋ１抑制劑之固體形式
CN112225736B (zh) * 2020-11-12 2022-04-15 山东省科学院菏泽分院 一种6-溴咪唑并[1.2-a]吡啶-3-甲醛的制备方法
US11912680B2 (en) 2021-12-28 2024-02-27 Empathbio, Inc. Nitric oxide releasing prodrugs of MDA and MDMA
PE20242346A1 (es) * 2022-01-07 2024-12-16 Horizon Therapeutics Ireland Dac Inhibidores heterociclicos de glut9 para el tratamiento de enfermedades
KR102879073B1 (ko) * 2022-09-02 2025-10-31 단국대학교 천안캠퍼스 산학협력단 트리플루오로메틸페닐 티아디아진계 화합물 및 이를 유효성분으로 포함하는 근감소증 예방 또는 치료용 조성물
CN117049961A (zh) * 2023-08-16 2023-11-14 苏州君叶生物医药科技有限公司 一种酵母脱氢酶抑制剂的衍生物及其合成方法

Family Cites Families (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW458977B (en) * 1997-04-16 2001-10-11 Abbott Lab 6,7-disubstituted-4-aminopyrido[2,3-D] pyrimidine compounds
WO2000040243A1 (en) 1999-01-08 2000-07-13 Smithkline Beecham Corporation Novel compounds
NZ513642A (en) 1999-01-21 2004-02-27 Metamorphix Inc Growth differentiation factor inhibitors and uses therefor
JP2001081087A (ja) * 1999-09-13 2001-03-27 Sankio Chemical Co Ltd 新規な２−（２−ピリジル）ピリミジン誘導体
WO2001057040A1 (en) * 2000-02-03 2001-08-09 Abbott Laboratories 6,7-disubstituted-4-aminopyrido[2,3-d]pyrimidine compounds
KR100804111B1 (ko) * 2000-08-11 2008-02-18 에자이 알앤드디 매니지먼트 가부시키가이샤 2-아미노피리딘 화합물 및 그의 의약 용도
EP1317433A2 (en) * 2000-09-06 2003-06-11 Chiron Corporation Inhibitors of glycogen synthase kinase 3
US7320789B2 (en) 2001-09-26 2008-01-22 Wyeth Antibody inhibitors of GDF-8 and uses thereof
AU2002343512B2 (en) * 2001-10-15 2007-12-06 E.I. Du Pont De Nemours And Company Iminobenzoxazines, iminobenzthiazines and iminoquinazolines for controlling invertebrate pests
WO2003082191A2 (en) * 2002-03-28 2003-10-09 Merck & Co., Inc. Substituted 2,3-diphenyl pyridines
FR2856684B1 (fr) * 2003-06-26 2008-04-11 Sanofi Synthelabo Derives de diphenylpyridine, leur preparation et leur application en therapeutique
US7470807B2 (en) 2003-08-14 2008-12-30 Asahi Kasei Pharma Corporation Substituted arylalkanoic acid derivatives and use thereof
ES2305887T3 (es) 2003-12-18 2008-11-01 Janssen Pharmaceutica Nv Derivados de pirido y pirimidopirimidinas como agentes antiproliferativos.
JP2007526324A (ja) * 2004-03-02 2007-09-13 スミスクライン・ビーチャム・コーポレイション Ａｋｔ活性のある阻害剤
ES2241496B1 (es) 2004-04-15 2006-12-01 Almirall Prodesfarma, S.A. Nuevos derivados de piridina.
US7777035B2 (en) 2005-06-22 2010-08-17 Chemocentryx, Inc. Azaindazole compounds and methods of use
WO2007076086A2 (en) * 2005-12-22 2007-07-05 Biogen Idec Ma Inc Tricyclic spiro compounds useful as transforming growth factor modulators
RU2485115C2 (ru) * 2006-07-14 2013-06-20 Новартис Аг Производные пиримидина в качестве ингибиторов alk-5
FR2904827B1 (fr) * 2006-08-11 2008-09-19 Sanofi Aventis Sa Derives de 5,6-bisaryl-2-pyridine-carboxamide, leur preparation et leur application en therapeutique comme antiganistes des recepteurs a l'urotensine ii
CA2667962A1 (en) 2006-10-30 2008-05-08 Novartis Ag Heterocyclic compounds as antiinflammatory agents
ES2303776B1 (es) * 2006-12-29 2009-08-07 Laboratorios Almirall S.A. Derivados de 5-fenil-6-piridin-4-il-1,3-dihidro-2h-imidazo(4,5-b)piridin-2-ona utiles como antagonistas del receptor de adenosina a2b.
US20100105714A1 (en) * 2007-01-30 2010-04-29 Biogen Idec Ma Inc. Furanone Compounds and Methods of Making and Using The Same
EP2134684B1 (en) * 2007-04-16 2017-08-02 AbbVie Inc. 7-substituted indole as mcl-1 inhibitors
BRPI0813625A2 (pt) 2007-07-26 2014-12-23 Novartis Ag Imidazo-[1,2b]-piridozinas 2,3,7-substituídos para tratamento de doenças mediadas por alzk4 ou alk5
WO2009032653A1 (en) * 2007-08-31 2009-03-12 Smith Kline Beecham Corporation Inhibitors of akt activity
MX2010002312A (es) 2007-08-31 2010-03-18 Merck Serono Sa Compuestos de triazolopiridina y su uso como inhibidores de cinasa reguladora de señal de apoptosis.
US20100227845A1 (en) * 2007-10-18 2010-09-09 Zhicai Wu Substituted 1,2,4-oxadiazoles and analogs thereof as cb2 receptor modulators, useful in the treatment of pain, respiratory and non-respiratory diseases
FR2927330B1 (fr) 2008-02-07 2010-02-19 Sanofi Aventis Derives de 5,6-bisaryl-2-pyridine-carboxamide, leur preparation et leur application en therapeutique comme antagonistes des recepteurs a l'urotensine ii
KR101015858B1 (ko) * 2008-06-26 2011-02-23 제일모직주식회사 유기 화합물, 및 이를 포함하는 유기 광전 소자
US8501940B2 (en) * 2008-07-15 2013-08-06 Hoffmann-La Roche Inc. Tetrahydrocinnoline derivatives
JP5731399B2 (ja) * 2008-12-30 2015-06-10 チェイル インダストリーズ インコーポレイテッド 新規な有機光電素子用化合物およびこれを含む有機光電素子
US8569316B2 (en) 2009-02-17 2013-10-29 Boehringer Ingelheim International Gmbh Pyrimido [5,4-D] pyrimidine derivatives for the inhibition of tyrosine kinases
SG181908A1 (en) * 2009-12-23 2012-08-30 Elan Pharm Inc Pteridinones as inhibitors of polo-like kinase
WO2011096196A1 (en) * 2010-02-02 2011-08-11 Oncotherapy Science, Inc. Lsd1 for target genes of cancer therapy and diagnosis
EP2531500B1 (en) * 2010-02-05 2018-01-24 Merck Patent GmbH Hetaryl-[1,8]naphthyridine derivatives
US8575203B2 (en) 2010-04-21 2013-11-05 Boehringer Ingelheim International Gmbh Chemical compounds
EP2590946B1 (en) * 2010-07-05 2015-02-18 Merck Patent GmbH Bipyridyl derivatives useful for the treatment of kinase-induced diseases
JP6457942B2 (ja) * 2012-10-05 2019-01-23 ライジェル ファーマシューティカルズ， インコーポレイテッド Ｇｄｆ−８阻害剤

Also Published As

Publication number Publication date
MA38050A1 (fr) 2016-06-30
MA38050B1 (fr) 2017-01-31
BR112015007182A2 (pt) 2017-07-04
EP2903978A1 (en) 2015-08-12
US9518040B2 (en) 2016-12-13
MX2015004151A (es) 2015-07-06
TN2015000121A1 (en) 2016-06-29
US20140107073A1 (en) 2014-04-17
US20170342048A1 (en) 2017-11-30
IL238031A0 (en) 2015-05-31
EP2903978B1 (en) 2022-12-07
AU2013326867B2 (en) 2018-03-08
JP2016500671A (ja) 2016-01-14
JP2019048841A (ja) 2019-03-28
US9878992B2 (en) 2018-01-30
CL2015000851A1 (es) 2015-08-28
SG11201502527UA (en) 2015-04-29
US20160052909A1 (en) 2016-02-25
AU2013326867A1 (en) 2015-05-21
CA2887203A1 (en) 2014-04-10
ZA201503041B (en) 2017-11-29
US9145433B2 (en) 2015-09-29
SA515360229B1 (ar) 2015-11-25
WO2014055955A1 (en) 2014-04-10
EA201590693A1 (ru) 2015-08-31
KR20150072412A (ko) 2015-06-29
CN104837832A (zh) 2015-08-12
PH12015500719A1 (en) 2015-05-18
CN104837832B (zh) 2019-04-26
JP6457942B2 (ja) 2019-01-23

Similar Documents

Publication Publication Date Title
PE20150767A1 (es) Inhibidores de gdf-8
PE20161246A1 (es) Acrilamidas de pirrolo[2,3-d]pirimidinilo, pirrolo[2,3-b]pirazinilo y pirrolo[2,3-d]piridinilo
DOP2015000158A (es) Inhibidores de prmt5 y sus usos
CL2011002955A1 (es) Compuestos derivados de 3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]octanonitrilo o heptanonitrilo o sus sales, como inhibidores de jak; procedimiento de preparacion; composicion farmaceutica que los comprende; utiles para el tratamiento de trastornos autoinmunes, cancer, entre otras enfermedades.
EA201691302A1 (ru) Новые гетероциклические соединения
EA201500298A1 (ru) Алкоксипиразолы в качестве активаторов растворимой гуанилатциклазы
GT201300174A (es) Compuestos de indol o análogos de los mismos útiles para el tratamiento de la degeneración macular relacionada con la edad (dme)
EA201400182A1 (ru) Производные пиридин-2(1н)-она в качестве ингибиторов jak
PE20151280A1 (es) Compuestos y metodos para la modulacion de quinasas y sus indicaciones
ECSP12012326A (es) Derivados de aminopirimidina como moduladores de la lrrk2
EA201592199A1 (ru) Производные бипиразола в качестве ингибиторов jak
UY32640A (es) Aril-pirimidinas como inhibidoras de sintasa dfe aldosterona
UY35675A (es) Derivados sustituidos de quinazolin-4-ona
EA201301319A1 (ru) Производные пиридин-2(1н)-она, применимые в качестве лекарственных средств для лечения миелопролиферативных нарушений, отторжения трансплантата, иммунологически обусловленных и воспалительных заболеваний
EA201370166A1 (ru) Содержащие диарилацетиленгидразид ингибиторы тирозинкиназы
PE20141598A1 (es) Derivados de dihidro-benzo-oxazina y dihidro-pirido-oxazina
JO3115B1 (ar) مركبات بيريدازينون واستخدامها كمثبطات daao
PH12016501624A1 (en) 1,2-substituted cyclopentanes as orexin receptor antagonists
EA201300250A1 (ru) Оксадиазольные ингибиторы продуцирования лейкотриена
MX392259B (es) ANILLOS 6-5 FUSIONADOS COMO INHIBIDORES C5a
PE20170946A1 (es) 2-amino-6-(difluorometil)- 5,5-difluoro-6-fenil-3,4,5,6-tetrahidropiridinas como inhibidores de bace1
EA201300436A1 (ru) Совместные кристаллы и соли ингибиторов ccr3
CO2019002618A2 (es) Compuestos de aza–indazol para usar en lesiones de tendones y/o ligamentos
CY1120133T1 (el) Πυριδαζινονες ως αναστολεις ενζυμου daao
EA201692300A1 (ru) Производные карбоксамида

Legal Events

Date Code Title Description
FD Application declared void or lapsed